Design, synthesis and evaluation of biological derivatives pyrroles potentially antiinflamatory activity / Planejamento, síntese e avaliação biológica de derivados pirrólicos com potencial atividade antiinflamatória

AUTOR(ES)
DATA DE PUBLICAÇÃO

2009

RESUMO

The nonsteroidal antiinflammatory drugs (NSAIDs) are among the most prescribed and used drugs in the world. These drugs inhibit the cyclooxygenases, enzymes responsible for conversion of arachidonic acid into phlogistic prostaglandins, by the action of phospholipase A2. The synthesis of compounds containing pyrrole nucleus in their structures has been a topic very attractive and well studied, that knowledge added to the site of interaction of the drug to the receptor enables the planning of new structures of substances candidates for prototypes of new drugs through of molecular modification. In this context, this work aimed at the design, synthesis and biological evaluation of pyrrole derivatives with potential antiinflammatory activity, based on the structures of indomethacin, the prototype of arylalkanoic acid class and diarylheterocycles (coxibs). Thus, five compounds were obtained in good yields from ethyl acetoacetate, route of Hantzsch and cyclofunctionalization methods, using ultrasound, which resulted in the reduction of the reaction time and consumption of solvent, following the principles of Green Chemistry. The 5a and 5b compounds were shown to be promising, from tests in vitro.

ASSUNTO(S)

inflamação (processos; estudo clínico) betaenaminoéster pirrol ultrasound inflammation pyrrol nonsteroidal antiinflammatory cyclofuncionalization betaenaminoester ultrassom ciclofuncionalização antiinflamatórios não-esteróides (estudo; atividade) planejamento de fármacos

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